Maniewska Jadwiga, Gąsiorowska Justyna, Szczęśniak-Sięga Berenika, Michalak Krystyna
Department of Chemistry of Drugs, Wroclaw Medical University, Wrocław, Poland.
Department of Biophysics, Wroclaw Medical University, Wrocław, Poland.
Acta Biochim Pol. 2018;65(2):185-191. doi: 10.18388/abp.2018_2604. Epub 2018 May 22.
The purpose of the present work was to assess the ability of five new oxicam analogues to interact with the lipid bilayers. To characterize the interaction of newly synthesized NSAIDs (non-steroidal anti-inflammatory drugs) analogues with DPPC lipid bilayers the two following techniques were applied - differential scanning calorimetry (DSC) and fluorescence spectroscopy. The results obtained by these experimental approaches show that new oxicams analogues interact with the lipid model membranes under consideration. As demonstrated both in calorimetric and spectroscopic studies, the greatest influence on the thermotropic properties of the lipid membrane and on the quenching of fluorescence of Laurdan and Prodan was exerted by a derivative named PR47 containing in its structure a two-carbon aliphatic linker with a carbonyl group, as well as bromine and trifluoromethyl substituents.
本研究的目的是评估五种新型昔康类似物与脂质双层相互作用的能力。为了表征新合成的非甾体抗炎药（NSAIDs）类似物与二棕榈酰磷脂酰胆碱（DPPC）脂质双层的相互作用，采用了以下两种技术——差示扫描量热法（DSC）和荧光光谱法。通过这些实验方法获得的结果表明，新型昔康类似物与所研究的脂质模型膜相互作用。如量热和光谱研究所示，对脂质膜热致性质以及劳丹（Laurdan）和普罗丹（Prodan）荧光猝灭影响最大的是一种名为PR47的衍生物，其结构中含有一个带有羰基的二碳脂肪族连接基，以及溴和三氟甲基取代基。
